The influence of surface modification on the cytotoxicity of PAMAM dendrimers
The influence of surface modification on the cytotoxicity of PAMAM dendrimers
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DOI：
10.1016/s0378-5173(02)00623-3
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发表时间：
2003-02-18
影响因子：
5.8
通讯作者：
D'Emanuele, A
中科院分区：
文献类型：
--
作者：
Jevprasesphant, R;Penny, J;D'Emanuele, A
用Caco-2细胞检测了表面修饰对PAMAM树枝状大分子细胞毒性的影响。通过在阳离子PAMAM树状大分子(G2、G3、G4)表面偶联月桂酰链或聚乙二醇2000来修饰树枝状大分子。未修饰的树状大分子对Caco-2细胞的杀伤作用，阳离子(全代)明显高于阴离子(半代)树枝状大分子，且随着大小(代)和浓度的增加而增加。表面修饰后，阳离子PAMAM树状大分子的细胞毒性显著降低，其中添加6个月桂酰基或4个聚乙二醇链对降低细胞毒性尤为有效。这种细胞毒性的降低被认为是由于连接的链减少/屏蔽了树枝状大分子表面的正电荷。基于树枝状大分子的递送系统的细胞毒性可能与母体树枝状大分子非常不同。(C)2002 Elsevier Science B.V.保留所有权利。
The influence of surface modification on the cytotoxicity of PAMAM dendrimers was examined using Caco-2 cells. Dendrimers were modified by conjugating either lauroyl chains or polyethylene glycol (PEG) 2000 onto the surface of cationic PAMAM dendrimers (G2, G3, G4).The cytotoxicity of unmodified dendrimers towards Caco-2 cells was appreciably higher for cationic (whole generation) compared with anionic (half generation) dendrimers and for both types increased with increasing size (generation) and concentration. A marked decrease in the cytotoxicity of cationic PAMAM dendrimers was noted when the surface was modified, with the addition of six lauroyl or four PEG chains being particularly effective in decreasing cytotoxicity. This decrease in cytotoxicity is thought to be due to a reduction/shielding of the positive charge on the dendrimer surface by the attached chains. The cytotoxicity of dendrimer-based delivery systems is likely to be very different from the parent dendrimer. (C) 2002 Elsevier Science B.V. All rights reserved.